Functionalised Pyrazoles through a Facile One-Pot Procedure from N-Tosyl-N-propargyl-hydrazine and Aryl Iodides or Vinyl Triflates
Functionalised Pyrazoles through a Facile One-Pot Procedure from N-Tosyl-N-propargyl-hydrazine and Aryl Iodides or Vinyl Triflates
复制标题
通过简单的一锅法从 N-甲苯磺酰基-N-炔丙基肼和芳基碘或乙烯基三氟甲磺酸酯官能化吡唑
作者：
S. Cacchi*;G. Fabrizi;A. Carangio
用一锅法合成了功能化的吡唑类化合物，总收率较高。该合成包括容易获得的N-甲苯磺酰基-N-炔丙基肼与芳基碘或乙烯基三氟甲磺酸酯的钯催化的偶联，所得N-甲苯磺酰基-N-（1-芳基/乙烯基-1-丙炔-3-基）肼的钯催化的环化，以及将由环化步骤产生的反应混合物暴露于KOBU t。
Functionalised pyrazoles have been prepared in good overall yield through a facile one-pot procedure. The synthesis includes the palladium-catalysed coupling of the readily available N-tosyl-N-propargylhydrazine with aryl iodides or vinyl triflates, the palladium-catalysed annulation of the resulting N-tosyl-N-(1-aryl/vinyl-1-propyn-3-yl) hydrazine and exposure of the reaction mixture arising from the annulation step to KOBu t.